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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
[Image: see text] The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a linker. Here we examined the impact of derivatizing two different BET bromodomain...
Gardado en:
| Publicado en: | J Med Chem |
|---|---|
| Main Authors: | , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado: |
American Chemical
Society
2017
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| Acceso en liña: | https://ncbi.nlm.nih.gov/pmc/articles/PMC5788402/ https://ncbi.nlm.nih.gov/pubmed/28595007 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01912 |
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